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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793180/insulin-is-a-potential-antioxidant-for-diabetes-associated-cognitive-decline-via-regulating-nrf2-dependent-antioxidant-enzymes
#2
Ying Song, Wei Ding, Yun Bei, Yan Xiao, Hai-Da Tong, Li-Bo Wang, Li-Yao Ai
PURPOSE: To investigate the neuroprotective effects of insulin on diabetic encephalopathy and its mechanism. EXPERIMENTAL AND APPROACH: The diabetic model was established by injection of streptozotocin. Behavior examinations were conducted by the Morris water maze. Histopathological alterations were detected by HE staining. ROS, CAT levels and SOD activity were measured using a microplate reader. In vitro, the viability of wild type and knock-down PC12 cells was detected by MTT assay, the morphology of cells was monitored under a microscope...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793051/promising-antileishmanial-activity-of-novel-imidazole-antifungal-drug-luliconazole-against-leishmania-major-in-vitro-and-in-silico-studies
#3
Azar Shokri, Mahdi Abastabar, Masoud Keighobadi, Saeed Emami, Mahdi Fakhar, Saeed Hosseini Teshnizi, Koichi Makimura, Ali Rezaei-Matehkolaei, Hassan Mirzaei
OBJECTIVES: Pentavalent antimonials have been used for the treatment of leishmaniasis for more than 70 years; however their toxicity limits their benefits. Unfortunately, the efficacy of the first line drugs has been decreased and resistance seems to be noticeable. Luliconazole is a new azole with unique effects on fungi which has not been tested on Leishmania parasites yet. METHODS: In the present study, we evaluated cytotoxicity and anti-leishmanial activities of Luliconazole on promastigotes and intracellular amastigotes of Leishmania major (L...
May 21, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29792951/an-analysis-of-variability-in-genome-organisation-of-intracellular-calcium-release-channels-across-insect-orders
#4
Bartlomiej J Troczka, Ewan Richardson, Rafael Homem, T G Emyr Davies
Using publicly available genomic data, combined with RT-PCR validation, we explore structural genomic variation for two major ion channels across insect classes. We have manually curated Ryanodine receptor (RyR) and inositol 1,4,5-trisphosphate receptor (IP3 R) ORFs and their corresponding genomic structures from 26 different insects covering major insect orders. We found that, despite high protein identity for both RyRs (>75%) and IP3 Rs (~67%), the overall complexity of the gene structure varies greatly between different insect orders with the simplest genes (fewest introns) found in Diptera and the most complex in Lepidoptera...
May 21, 2018: Gene
https://www.readbyqxmd.com/read/29792932/cystine-glutamate-transporter-system-x-c-is-involved-in-nitric-oxide-production-in-mouse-peritoneal-macrophages
#5
Sho Kobayashi, Shinji Hamashima, Takujiro Homma, Mami Sato, Ryosuke Kusumi, Shiro Bannai, Junich Fujii, Hideyo Sato
The amino acid transport system xc - is important for maintaining intracellular glutathione levels and extracellular redox balance. The main component of system xc - , xCT, is strongly induced by various stimuli, including oxidative stress and bacterial lipopolysaccharides (LPS) in macrophages. In the present study, we investigated the production of nitric oxide by LPS-stimulated mouse peritoneal macrophages isolated from both xCT-deficient and wild-type mice. After culturing macrophages in the presence of LPS for 24-48 h, nitrite levels in the medium of xCT-deficient macrophages were significantly decreased compared to that of wild-type cells...
May 21, 2018: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29792841/decarboxylation-of-ang-1-7-to-ala-1-ang-1-7-leads-to-significant-changes-in-pharmacodynamics
#6
Anja Tetzner, Maura Naughton, Kinga Gebolys, Jenny Eichhorst, Esther Sala, Óscar Villacañas, Thomas Walther
The heptapeptide angiotensin (Ang)-(1-7) is part of the beneficial arm of the renin-angiotensin system. Ang-(1-7) has cardiovascular protective effects, stimulates regeneration, and opposes the often detrimental effects of Ang II. We recently identified the G protein-coupled receptors Mas and MrgD as receptors for the heptapeptide. Ala1 -Ang-(1-7) (Alamandine), a decarboxylated form of Ang-(1-7), has similar vasorelaxant effects, but has been described to only stimulate MrgD. Therefore, this study aimed to characterise the consequences of the lack of the carboxyl group in amino acid 1 on intracellular signalling and to identify the receptor fingerprint for Ala1 -Ang-(1-7)...
May 21, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29792817/macroscopic-theory-for-evolving-biological-systems-akin-to-thermodynamics
#7
Kunihiko Kaneko, Chikara Furusawa
We present a macroscopic theory to characterize the plasticity, robustness, and evolvability of biological responses and their fluctuations. First, linear approximation in intracellular reaction dynamics is used to demonstrate proportional changes in the expression of all cellular components in response to a given environmental stress, with the proportion coefficient determined by the change in growth rate as a consequence of the steady growth of cells. We further demonstrate that this relationship is supported through adaptation experiments of bacteria, perhaps too well as this proportionality is held even across cultures of different types of conditions...
May 20, 2018: Annual Review of Biophysics
https://www.readbyqxmd.com/read/29792687/co-mobility-of-gabarap-and-phosphatidylinositol-4-kinase-2a-on-cytoplasmic-vesicles
#8
Yan Chen, Hui-Qiao Sun, John P Eichorst, Joseph P Albanesi, Helen Yin, Joachim D Mueller
We previously reported that recruitment of the Type IIA phosphatidylinositol 4-kinase (PI4K2A) to autophagosomes by GABARAP, a member of the Atg8 family of autophagy-related proteins, is important for autophagosome-lysosome fusion. Because both PI4K2A and GABARAP have also been implicated in the intracellular trafficking of plasma membrane receptors in the secretory/endocytic pathway, we characterized their interaction in cells under non-autophagic conditions. Fluorescence fluctuation spectroscopy measurements revealed that GABARAP exists predominantly as a cytosolic monomer in live cells, but is recruited to small cytoplasmic vesicles upon overexpression of PI4K2A...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29792682/calix-4-arene-based-redox-sensitive-molecular-probe-for-sers-guided-recognition-of-labile-iron-pool-in-tumor-cells
#9
Padincharapad Sreedevi, Jyothi B Nair, Preethanuj Preethalayam, Benadicta S Jeeja, Cherumuttathu H Suresh, Kaustabh Kumar Maiti, Ramavarma Luxmi Varma
Targeting the intracellular 'labile' iron pool is turned as a key modulator for cancer progression since the former is responsible for several pathological processes in tumor cells. Herein, we report a non- fluorescent calix[4]arene based triazole appended molecular probe (PTBC) for redox-specific detection of Fe3+ under physiological condition by UV-vis, FT-IR, 1H NMR, HR-MS spectroscopies, ITC and the binding strategy between Calix[4]arene and Fe3+ was modeled by DFT calculations. As a new insight PTBC probe showed significant Raman fingerprint through surface enhanced Raman scattering (SERS) modality revealing the ultrasensitive detection of Fe3+ with a LOD of 2 nM...
May 24, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29792530/manganese-transport-and-toxicity-in-polarized-wif-b-hepatocytes
#10
Khristy J Thompson, Jennifer Hein, Andrew Baez, Jose Carlo Sosa, Marianne Wessling-Resnick
Mn toxicity arises from nutritional problems, community and occupational exposures, and genetic risks. Mn blood levels are controlled by hepatobiliary clearance. The goals of this study were to determine the cellular distribution of Mn transporters in polarized hepatocytes, to establish an in vitro assay for hepatocyte Mn efflux, and to examine possible roles the Mn transporters would play in metal import and export. For these experiments, hepatocytoma WIF-B cells were grown for 12-14 days to achieve maximal polarity...
May 24, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29792526/phages-antibiotic-resistance-are-the-most-abundant-entities-on-earth-ready-for-a-comeback
#11
Colin Hill, Susan Mills, Reynolds P Ross
Bacteriophages, which lost out to antibiotic therapy in the past, may be poised to make a comeback. Once discarded because of their narrow activity spectrum, it can now be viewed as a major advantage that these intracellular, self-replicating entities can exert their killing effect with minimal damage to the commensal microbiome. In eastern Europe, phages continue to be used both prophylactically and therapeutically to treat infections. More recently, much needed regulated clinical trials are underway with a view to restoring phage therapy as a tool for mainstream medicine, although current regulations may impede their full potential...
May 24, 2018: Future Microbiology
https://www.readbyqxmd.com/read/29792435/measuring-drug-induced-changes-in-metabolite-populations-of-live-bacteria-real-time-analysis-by-raman-spectroscopy
#12
Paul R Carey, Grant R Whitmer, Michael J Yoon, Michael N Lombardo, Marianne Pusztai-Carey, Hossein Heidari-Torkabadi, Tao Che
Raman difference spectroscopy is shown to provide a wealth of molecular detail on changes within bacterial cells caused by infusion of antibiotics or hydrogen peroxide. E. coli strains paired with chloramphenicol, DHFR propargyl-based inhibitors, meropenem, or hydrogen peroxide provide details of the depletion of protein and nucleic acid populations in real time. Additionally, other reproducible Raman features appear and are attributed to changes in cell metabolite populations. An initial candidate for one of the metabolites involves population increases of citrate, an intermediate within the TCA cycle...
May 24, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29792194/comparison-of-aqueous-polyethylene-glycol-aqueous-and-ethanolic-propolis-extracts-antioxidant-and-mitochondria-modulating-properties
#13
Loreta Kubiliene, Aiste Jekabsone, Modestas Zilius, Sonata Trumbeckaite, Daiva Simanaviciute, Rima Gerbutaviciene, Daiva Majiene
BACKGROUND: Propolis is multicomponent substance collected by honeybees from various plants. It is known for numerous biological effects and is commonly used as ethanolic extract because most of active substances of propolis are ethanol-soluble. However, water-based propolis extracts could be applied more safely, as this solvent is more biocompatible. On the other hand, water extracts has significantly smaller range and quantity of active compounds. The extraction power of water could be enhanced by adding co-solvent which increases both solubility and penetration of propolis compounds...
May 23, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29792156/design-synthesis-and-biological-evaluation-of-1h-1-2-3-triazole-linked-1h%C3%A2-dibenzo-b-h-xanthenes-as-inductors-of-ros-mediated-apoptosis-in-the-breast-cancer-cell-line-mcf-7
#14
Carolina S Bortolot, Luana da S M Forezi, Roberta K F Marra, Marcelo I P Reis, Barbara V F E Sa, Ricardo Imbroisi Filho, Zeinab Ghasemishahrestani, Mauro Sola-Penna, Patricia Zancan, Vitor F Ferreira, Fernando de C da Silva
BACKGROUND: Low molecular weight 1,2,3-triazoles and naphthoquinones are endowed with various types of biological activity, such as against cancer, HIV and bacteria. However, in some cases, the conjugation of these two nuclei considerably increases their biological activities Objective: In this work, we decided to study the synthesis and screening of bis-naphthoquinones and xanthenes tethered to 1,2,3-triazoles against cancer cell lines, specifically the human breast cancer cell line MCF-7...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792152/sorbinil-an-aldolase-reductase-inhibitor-in-fighting-against-diabetic-complications
#15
Qi Huang, Qiong Liu, Dongsheng Ouyang
BACKGROUND: Aldose reductase (AR) is involved in pathogenesis of diabetes, which is one of the major threats to global public health. OBJECTIVE: In this review article, we have discussed the role of sorbinil, an AR inhibitor (ARI), in preventing diabetic complications. RESULTS: AR contributes in diabetes by generating excess intracellular superoxide and other mediators of oxidative stress through polyol pathway. Inhibition of AR activity thus might be potential approach for the management of diabetic complications...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792023/fern-9-11-ene-2%C3%AE-3%C3%AE-diol-action-on-insulin-secretion-in-hyperglycemic-conditions
#16
Allisson Jhonatan Gomes Castro, Luisa Helena Cazarolli, Gabrielle Da Luz, Delsi Altenhofen, Hemily Batista Da Silva, Francieli Kanumfre Carvalho, Moacir Geraldo Pizzolatti, Fátima Rmb Silva
The objective of this study was to investigate the effect and the mechanism of action of fernenediol as insulin secretagogue. Wistar rats were treated with 0.1; 1 and 10 mg/kg fernenediol and then induced hyperglycemia by oral glucose. The glycaemia, insulin, LDH, calcium and hepatic glycogen were analyzed. Considering the intestine and pancreas as targets for the triterpene action, the duodenum was used to verify the influence of fernenediol on intestinal glycosidases. Additionally, pancreatic islets were used for studies of 14 C-deoxyglucose uptake and influx of 45 Ca2+ in hyperglycemic medium with/without fernenediol in the presence/absence of an inhibitor/activator of KATP channels, glibenclamide, diazoxide, nifedipine, calcium chelator (BAPTA- AM) and H-89 and ST the inhibitors of the PKA and PKC enzymes...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29791845/equilibrative-nucleoside-transporter-3-regulates-t-cell-homeostasis-by-coordinating-lysosomal-function-with-nucleoside-availability
#17
Chin-Wen Wei, Chia-Ying Lee, Ding-Jin Lee, Chang-Feng Chu, Ju-Chu Wang, Tien-Chiao Wang, Wann-Neng Jane, Zee-Fen Chang, Chuen-Miin Leu, Ivan L Dzhagalov, Chia-Lin Hsu
T cells are a versatile immune cell population responding to challenges by differentiation and proliferation followed by contraction and memory formation. Dynamic metabolic reprogramming is essential for T cells to meet the biosynthetic needs and the reutilization of biomolecules, processes that require active participation of metabolite transporters. Here, we show that equilibrative nucleoside transporter 3 (ENT3) is highly expressed in peripheral T cells and has a key role in maintaining T cell homeostasis by supporting the proliferation and survival of T cells...
May 22, 2018: Cell Reports
https://www.readbyqxmd.com/read/29791792/normalizing-tumor-microenvironment-based-on-photosynthetic-abiotic-biotic-nanoparticles
#18
Diwei Zheng, Bin Li, Lu Xu, Qiu-Ling Zhang, Jin-Xuan Fan, Chu-Xin Li, Xian-Zheng Zhang
Tumor hypoxia has attained the status of a core hallmark of cancer that globally affected the entire tumor phenotype. Reversing tumor hypoxia might offer alternative therapeutic opportunities for current anticancer therapies. In this research, a Photosynthetic Leaf-inspired Abiotic/biotic Nano-Thylakoid (PLANT) system was designed by fusing thylakoid membrane with synthetic nanoparticles for efficient O2 generation in vivo. Under 660 nm laser irradiation, PLANT system exhibited intracellular O2 generation and the anaerobic respiration of multicellular tumor spheroid was suppressed by PLANT as well...
May 23, 2018: ACS Nano
https://www.readbyqxmd.com/read/29791783/in-silico-and-wet-bench-interactomics-sheds-light-on-the-similitudes-and-differences-between-human-roco-proteins
#19
Jean-Marc Taymans, Marie-Christine Chartier-Harlin
Defining a common and specific functions for homologs of a novel protein family is not a trivial task. In their recent study, Tomkins and colleagues have addressed this challenge for the ROCO protein family by exploring interactomes of its four human members: MASL1, DAPK1, LRRK1 and LRRK2. ROCO proteins are characterized by a Ras-GTPase domain embedded in complex multidomain proteins and a functional descriptor for this protein family has been elusive despite accumulating research, particularly for LRRK2, a protein implicated in Parkinson's disease...
May 23, 2018: Proteomics
https://www.readbyqxmd.com/read/29791754/atp-triggers-a-robust-intracellular-ca-2-mediated-signalling-pathway-in-human-synovial-fibroblasts
#20
Kondo C, R B Clark, T Y Kim, Belke D, Banderali U, R T Szerencsei, A H Jalloul, P P M Schnetkamp, Spitzer Kw, Giles Wr
NEW FINDINGS: What is the central question of this study? In human articular joints, the synovial fibroblast HSF cell population has essential functions including secretion of lubricants. We address some remaining questions concerning activation-secretion coupling by characterizing the main [Ca2+ ]i signalling pathways activated by ATP. What is the main finding and its importance? In HSF ATP acts through a linked G-protein (Gq ) and phospholipase C signalling mechanisms to produce IP-3 which markedly enhances release of Ca2+ from the endoplasmic reticulum...
May 23, 2018: Experimental Physiology
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